TY - JOUR
T1 - Palladium (0) olefin complexes bearing purine-based N-heterocyclic carbenes and 1,3,5-triaza-7-phosphaadamantane (PTA)
T2 - Synthesis, characterization and antiproliferative activity toward human ovarian cancer cell lines
AU - Scattolin, Thomas
AU - Pangerc, Nicola
AU - Lampronti, Ilaria
AU - Tupini, Chiara
AU - Gambari, Roberto
AU - Marvelli, Lorenza
AU - Rizzolio, Flavio
AU - Demitri, Nicola
AU - Canovese, Luciano
AU - Visentin, Fabiano
PY - 2019/10/30
Y1 - 2019/10/30
N2 - A complete series of new η2-olefin palladium (0) complexes bearing purine-based N-heterocyclic carbenes or PTA (1,3,5-triaza-7-phospaadamantane) as spectator ligands have been synthetized and exhaustively characterized. The first single-crystal X-ray structure of a PTA complex of palladium (0) have been also reported. The most part of these compounds have been tested as antiproliferative agents toward two different human ovarian cancer cell lines A2780 and A2780cis, respectively cisplatin sensitive and resistant. The resulting IC50 values have shown the significant antiproliferative activity of our complexes, often comparable with cisplatin. In some cases, this cytotoxicity is associate with induction of apoptosis. The efficiency of the Pd (0) complexes is heavily influenced by the combination of spectator ligands and coordinating olefin. Finally, two of the most active compounds against cancer cells proved scarcely active on non-tumor fibroblast cells MRC-5.
AB - A complete series of new η2-olefin palladium (0) complexes bearing purine-based N-heterocyclic carbenes or PTA (1,3,5-triaza-7-phospaadamantane) as spectator ligands have been synthetized and exhaustively characterized. The first single-crystal X-ray structure of a PTA complex of palladium (0) have been also reported. The most part of these compounds have been tested as antiproliferative agents toward two different human ovarian cancer cell lines A2780 and A2780cis, respectively cisplatin sensitive and resistant. The resulting IC50 values have shown the significant antiproliferative activity of our complexes, often comparable with cisplatin. In some cases, this cytotoxicity is associate with induction of apoptosis. The efficiency of the Pd (0) complexes is heavily influenced by the combination of spectator ligands and coordinating olefin. Finally, two of the most active compounds against cancer cells proved scarcely active on non-tumor fibroblast cells MRC-5.
KW - 1,3,5-triaza-7-phosphaadamantane (PTA)
KW - Antiproliferative and proapototic activity
KW - Organometallic anticancer compounds
KW - Palladium(0) olefin complexes
KW - Purine-based N-heterocyclic carbenes
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U2 - 10.1016/j.jorganchem.2019.07.008
DO - 10.1016/j.jorganchem.2019.07.008
M3 - Article
AN - SCOPUS:85070487219
VL - 899
JO - Journal of Organometallic Chemistry
JF - Journal of Organometallic Chemistry
SN - 0022-328X
M1 - 120857
ER -